BMS-688521
目录号: PL14874 纯度: ≥98%
CAS No. :893397-44-9
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中文名称
BMS-688521
英文名称
BMS-688521
英文别名
BMS-688521;6-[(5S,9R)-9-(4-cyanophenyl)-3-(3,5-dichlorophenyl)-1-methyl-2,4-dioxo-1,3,7-triazaspiro[4.4]nonan-7-yl]pyridine-3-carboxylic acid;6-[(5S,9R)-9-(4-Cyanophenyl)-3-(3,5-dichlorophenyl)-1-methyl-2,4-dioxo-1,3,7-triazaspiro[4.4]non-7-yl]-3-pyridinecarboxylic acid (ACI);BMS 688521
Cas No.
893397-44-9
分子式
C26H19Cl2N5O4
分子量
536.37
包装储存
Powder -20°C 3 years;In solvent -80°C 6 months
产品详情
BMS-688521 是一种高效、具有口服活性的 LFA-1/ICAM 相互作用抑制剂,在粘附试验中 IC50 为 2.5 nM,在 MLR 试验中 IC50 为 60 nM。BMS-688521 对小鼠变应性嗜酸性肺炎模型有较好的研究作用。
生物活性
BMS-688521 is a highly potent, orally active inhibitor of the LFA-1/ICAM interaction, with an IC 50 of 2.5 nM in the adhesion assay and an IC 50 of 60 nM in the MLR assay. BMS-688521 is efficacious in a mouse allergic eosinophilic lung inflammation model.
性状
Solid
体外研究(In Vitro)
BMS-688521 in a mouse specific adhesion assay employed mouse splenocytes and a mouse ICAM-1 expression cell line, b.END3. BMS-688521 has an IC50 of 78 nM, representing an approximately 30-fold decrease in activity relative to the human T-cell/HUVEC assay data (ICIC50=2.5 nM). has not independently confirmed the accuracy of these methods. They are for reference only.
体内研究(In Vivo)
BMS-688521 (1-10 mg/kg; p.o.; BID for a three-day) is efficacious in a mouse allergic eosinophilic lung inflammation model.
BMS-688521 (5 mg/kg; p.o.) treatment shows the C max , T max , AUC, F values are 0.32 μM, 1.0 μM, 1.5 μM h, and 50%, respectively.
BMS-688521 (1 mg/kg; i.v.) treatment shows the T 1/2 , MRT, CL and Vss values are 1.6 hours, 1.7 hours, 50 mL/mim/kg, and 5.1 L/kg, respectively in BALB/c mice. has not independently confirmed the accuracy of these methods. They are for reference only.
运输条件
Room temperature in continental US; may vary elsewhere.
储存方式
Powder -20°C 3 years;In solvent -80°C 6 months
参考文献
[1]. Watterson SH, et al. Small molecule antagonist of leukocyte function associated antigen-1 (LFA-1): structure-activity relationships leading to the identification of 6-((5S,9R)-9-(4-cyanophenyl)-3-(3,5-dichlorophenyl)-1-methyl-2,4-dioxo-1,3,7-triazaspiro[4
溶解度数据
In Vitro: DMSO : 100 mg/mL (186.44 mM; Need ultrasonic)配制储备液
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1:一般建议:溶解度为Medlife测试数据,可能与文献描述存在差异。这是由于生产工艺和批次不同产生的正常现象。为了使其更好的溶解,请用37℃加热试管并在超声波水浴中震动片刻。不同批次产品溶解度各有差异,仅做参考,具体以实验方案为准。

2:储存条件:粉末-20°C一般情况可以保存3年,溶于溶剂-80°C一般情况可以保存1年。不同产品及不同批次产品可能存在差异,请细致阅读产品信息,并辅助参考相关文献描述。

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